Oral administration of fructose for alcohol intoxication

ABSTRACT

ORAL ADMINSTRATION OF LOZENGES CONTAINING ABOUT 500 MG. TO ABOUT 1500 MG. OF CRYSTALLINE, HIGHLY PRIFIED FRUCTOSE TO ACCELERATE DEXTOXICATION OF AN INTOXICATED SUBJECT IS DESCRIBED.

United States Patent ABSTRACT OF THE DISCLOSURE Oral administration of lozenges containing about 500 mg. to about 1500 mg. of crystalline, highly purified fructose to accelerate detoxication of an intoxicated subject is described.

This invention relates to fructose-containing lozenges and their oral use to accelerate reduction of the alcohol concentration in the blood of a subject.

'Over the years a substantial number of scientific studies have been reported in the literature concerning the decline of alcohol concentration in the blood of a patient under the action of fructose. These studies were reportedly carried out by administering the fructose intravenously or orally. In carrying out such oral studies the dose of fructose is dissolved in a liquid e.g. water, and then ingested orally by a subject (human being) weighing at least about 50 kg. In such studies at least 50 grams of fructose were administered in a single dose on the basis of at least 1 g./kg. of body weight and such dose was repeated at one hour intervals in many cases. These large doses were reported to cause nausea, heat sensation, flushing and epigastric pain.

It has now been found that a rapid lowering of the alcohol concentration in the blood after oral ingestion of alcohol can now be achieved without any side effects by the oral administration of lozenges containing a substantially pure, crystalline fructose, using a substantially lower dose of fructose than heretofore reported in the prior art.

Accordingly, one aspect of the present invention relates to the oral administration of fructose lozenges which provide accelerated detoxication of a subject upon the administration of about mg. to about 100 mg./kg. of body weight.

Another aspect of the present invention relates to fructose tablets which do not cause any side effects heretofore associated with the administration of fructose.

Still another aspect of the present invention relates to a tablet containing about 500 mg. to about 1500 mg. of substantially pure crystalline fructose, this tablet exhibiting slow release characteristics.

These and other aspects of the present invention will become apparent from the following description.

The fructose used in the present invention is preferably a crystalline material of very high purity, i.e. at least 98%. Other sugars such as glucose and glucose containing compounds are preferably not present in the fructose used in accordance with the invention. Exemplary of a suitable fructose is one which conforms to N.F. food grade (D levulose). The preferred fructose em ployed has a molecular weight of about 180, a decomposition temperature of 103-105 C., a specific rotation [a] of 91.8 to 93.8 and a moisture content of less than 0.1%. Such a material may be prepared in accordance with the process described in U.S. Patent 2,949,389.

It has been found desirable to formulate the fructose into a solid form such as a lozenge tablet or the like.

3,584,122 Patented June 8, 1971 In the preparation of such a tablet the fructose may be formulated with other ingredients in accordance with conventional procedures employing solid carriers, e.g. starch, sugar, bentonite; lubricants, e.g. magnesium stearate. It also is desirable to include a hydroscopic agent, e.g. dicalcium phosphate dihydrate, and a binder preferably polyvinyl pyrrolidone. Each fructose tablet contains about 500 mg. to about 1500 mg. fructose, preferably 1000 mg.

The following example is illustrative of the preparation of a solid lozenge in accordance with the present invention.

Tablets were prepared with the following:

Ingredients: Mg. per tablet Fructose (N.F. food grade available from Dawes Laboratories, Inc.) 1000 Polyvinyl pyrrolidone l0 Dicalcium phosphate dihydrate 10 Cabosil M-S 2.4 Flavoring agent 5 Magnesium stearate 10 Talc 20 All of the components were blended together, screened and then compressed into tablets of appropriate size and weight using a suitable tablet compression machine.

Studies were carried out with human subjects to determine the concentration of ethanol in the blood following a standard dose of 1 oz. of -proof vodka spirit, after the oral administration of fructose.

The subjects employed were instructed to have a light breakfast relatively free of fat. About an hour after breakfast each subject received 30 ml. of the vodka with a side glass of water both of which were swallowed within five minutes. In addition, half of the subjects were given two lozenges of fructose, each containing 1 gram, to suck and swallow as they dissolved.

Following the drinking of the alcohol venous blood was drawn from all the subjects using Zephiran solution as an antiseptic to cleanse the site of the puncture. Sodium fluoride was used as the anticoagulant and the analysis of the blood was begun immediately. Alcohol content of the blood was determined by the Conway diffusion dish method. Blood was drawn at 30, 60 and minutes following the drinking of the alcohol.

A week later the same procedure was repeated with the same subjects. The subjects who had previously received the fructose lozenges received none this time and those who had not reecived the fructose lozenges now received such lozenges.

Following the last blood sample from each subject, all the subjects were observed for symptoms suggestive of alcohol effect until evening.

It was found that the alcohol content of the blood following the sucking of two l-gram lozenges of fructose was less than .05% at 60 minutes whereas the alcohol content of those subjects not receiving any fructose was about 0.20 to 0.25%.

In all of the subjects including those receiving the fructose, the alcohol content at 30 minutes was between about 0.10% and 0.20%. This data indicates that a substantial reduction in the alcohol content of the blood was achieved at 60 minutes after taking of the fructose tablet and it was found to be further accelerated at 90 minutes.

Under guidelines established by the National Safety Council for the determination of a person under the influence of alcohol the following criteria have been set up.

(1) Less than 0.05%prirna facie evidence that the subject is not under the influence of alcohol.

(2) 0.05-0.15%corroborative evidence to be con sidered with outward physical symptoms.

(3) 0.15% and aboveprima facie evidence that the subject is under the influence of alcohol.

(4) 0.25% and above-the subject is markedly intoxicated.

Thus employing the following guidelines, the subjects receiving the fructose within 60 minutes after the administration of two l-gm. tablets of fructose, had the alcohol concentration in their blood reduced to a level considered to be prima facie evidence that the subject is not under the influence of alcohol.

Various modifications of the compositions of the invention may be made without departing from the spirit or scope thereof and it is to be understood that the invention is to be limited only as defined in the appended claims.

What is claimed is:

1. The method of reducing alcohol concentration in humans due to the ingestion of alcohol which comprises placing in the oral cavity a solid composition containing an effective dose of crystalline fructose in substantially pure form and a solid pharmaceutical carrier, said effec- 4 tive dose of fructose comprising about 10 mg. to about 100 mg. per kilogram of body weight and permitting said solid composition to dissolve in said oral cavity.

2. The method, according to claim 1, wherein said human receiving said fructose is intoxicated.

3. The method of increasing the tolerance to alcohol ingestion in a human which comprises placing in the oral cavity a tablet containing an effective dose of a crystalline fructose in a substantially pure form, said effective dose comprising about 10 mg. to about 100 mg. per kilogram of body weight of said fructose and permitting said tablet to dissolve in said oral cavity.

4. The method according to claim 3 wherein said tablet contains from about 500 mg. to about 1500 mg. of said fructose.

References Cited Lundquist et al., Acta Pharmacol, vol. 14, pp. 290- 294, 1958.

RICHARD L. HUFF, Primary Examiner 

